绞股蓝总苷对正常与高脂血症大鼠体内CYP3A2酶活性影响的差异性研究OA

To evaluate the effect of gypenosides(Gyps)on CYP3A2 enzyme activity in normal and hyperlipidemia rats by probe drug method.Methods:The experimental animals were divided into normal rats control group,normal rats Gyps group,hyperlipidemia rats control group,and hyperlipidemia rats Gyps group.The animals in control and Gyps groups were given blank solvent and Gyps for 7 days respectively.On the 8th day,the rats in each groups were given the probe drug(aminopterin).The effect of Gyps on CYP3A2 activity in normal and hyperlipidemic rats was analyzed by detecting blood concentration of probe drug using HPLC method and calculating pharmacokinetic parameters.Results:Compared with normal rats control group and hyperlipidemia rats control group,AUC,Cmax of dapsone increased,t1/2 was significantly prolonged,and CLz/F significantly decreased both in normal rats Gyps group and hyperlipidemia rats Gyps group(P<0.01).Compared with normal rats control group,AUC of dapsone in hyperlipidemia rats control group significantly increased and the CLz/F significantly decreased(P<0.01).After administration of Gyps,compared with normal rats Gyps group,the increase of AUC and decrease of CLz/F of dapsone in hyperlipidemia rats Gyps group were more significant(P<0.01).Conclusion:The activity of CYP3A2 enzyme in rats can be inhibited by Gyps.The results suggest that the dosage of drug should be adjusted to avoid the potential risk of herb-drug interactions when Gyps is combined with drugs metabolized by CYP3A4,especially in hyperlipidemia.